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Analogs of terpene trilactones from Ginkgo biloba and related compounds and uses thereof
   
Document Number
US Patent 7145021
Issued Date
December 5, 2006
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Abstract
The subject invention provides compounds having the structure: ##STR00001## wherein R.sub.1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R.sub.2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R.sub.3 is H or OH; R.sub.4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C.sub.1 C.sub.5) alkyl group, (C.sub.2 C.sub.5) alkenyl, or a (C.sub.2 C.sub.5) alkynyl, (C.sub.1 C.sub.5) alkoxy, (C.sub.2 C.sub.5) alkenyloxy, or (C.sub.2 C.sub.5) alkynyloxy, --N3, --COR5, --CONR5R6, --CO2R5, --OCOR5, --NH(OH), --NR5R6, --NHCOR5, --N(OH)COR5, --CH2OR5, --OCH2CO2R5, --CH2SR5, --CH2NR5R6, --SR5, --OSR5, or --NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C.sub.1 C.sub.5) alkyl, (C.sub.2 C.sub.5) alkenyl, or (C.sub.2 C.sub.5) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1 C10) alkyl, (C1 C10) alkenyl, (C1 C10) alkynyl, -A-Ar, -A-Z-Ar, --SO.sub.2--Ar, or -A-NR.sub.5, or --R.sub.7, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject.
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Number of Claims:
34
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Published
December 5, 2006
Application Number
10/401,931
Filed
March 28, 2003
US Classification
549/297   544/335 546/164 546/284.1
Int'l Classification
C07D   307/77   (20060101)  
Examiner
Parent Case
RELATED COMPOUNDS AND USES THEREOF This application is a continuation-in-part of U.S. Ser. No. 10/109,965, filed Mar. 29, 2002, now U.S. Pat. No. 6,693,091, issued Feb. 17, 2004, and also claims the benefit of U.S. Provisional Application No. 60/436,916, filed Dec. 27, 2002, the entire contents of both are hereby incorporated by reference.
USPTO Field of Search
514/256   514/338.8   514/314   514/468   549/297   546/164   546/284.1   544/335  
Related Patents
7473788 - Analogs of terpene trilactones from Ginkgo biloba and related compounds and uses thereof - Owned by The Trustees of Columbia University in the City of New York (New York, NY)

The subject invention provides compounds having the structure: ##STR00001## wherein R.sub.1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R.sub.2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R.sub.3 is H or OH; R.sub.4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C.sub.1-C.sub.5) alkyl group, (C.sub.2-C.sub.5) alkenyl, or a (C.sub.2-C.sub.5) alkynyl, (C.sub.1-C.sub.5) alkoxy, (C.sub.2-C.sub.5) alkenyloxy, or (C.sub.2-C.sub.5) alkynyloxy, --N3, --COR5, --CONR5R6, --CO2R5, --OCOR5, --NH(OH), --NR5R6, --NHCOR5, --N(OH)COR5, --CH2OR5, --OCH2CO2R5, --CH2SR5, --CH2NR5R6, --SR5, --OSR5, or --NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C.sub.1-C.sub.5) alkyl, (C.sub.2-C.sub.5) alkenyl, or (C.sub.2-C.sub.5) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1-C10) alkyl, (C1-C10) alkenyl, (C1-C10) alkynyl, -A-Ar, -A-Z-Ar, --SO.sub.2--Ar, or -A-NR.sub.5, or --R.sub.7, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject.

7429670 - Synthesis of derivatives of ginkgolide C - Owned by The Trustees of Columbia University in the City of New York (New York, NY)

The subject invention provides ginkgolide C derivatives compounds having the structure: ##STR00001## wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, --CH.sub.2CO.sub.2R.sup.4, and --CH.sub.2CONR.sup.5R.sup.6; where R.sup.4 is an alkyl group; and R.sup.5 and R.sup.6 are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R.sup.1 is H or --COR.sup.7, where R.sup.7 is alkyl, aryl or amino; wherein R.sup.2 is present or absent, and when present is H, --COR.sup.8 or --CO--Z--R.sup.8; where R.sup.8 is alkyl, aryl or amino; and Z is oxygen; wherein R.sup.3 is present or absent, and when present is --COR.sup.9; where R.sup.9 is alkyl or aryl; wherein only one of R.sup.2 or R.sup.3 is present in the compound; wherein only two of R, R.sup.1, R.sup.2 and R.sup.3 are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R.sup.3 is absent and bond b is present when R.sup.2 is absent; or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.

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